General Information

General Information

DRAVP ID DRAVPe00573

Peptide Name HR2P-M2

Sequence SLTQINTTLLDLEYEMKKLEEVVKKLEESYIDLKEL

Sequence Length 36

UniProt ID No entry found

Taxon ID None

Source Synthetic construct

Validation Experimentally Validated

Origin Information

Gene Name/ID Not Available

GenBank Not Available

Amino Acid position Not Available

Domain Accession ID Not Available

Nucleotide sequence ID Not Available

Molecular Type Not Available

Chromosomal Position Not Available

Activity Information

Target Organism MERS-CoV

Assay Inhibition of MERS-CoV S-Protein-Mediated Cell–Cell Fusion Assay

Activity

[Ref.29442512]MERS-CoV:inhibition of cell-cell fusion in Huh-7 cells(EC50=0.75 ± 0.09 μM);
WT MERS-CoV pseudovirus:inhibition of pseudovirus infection in calu-3 cells(EC50=1.07±0.21 μM);
Q1020H-MERS-CoV pseudovirus:inhibition of pseudovirus infection in calu-3 cells(EC50=1.25± 0.18 μM);
Q1020R-MERS-CoV pseudovirus:inhibition of pseudovirus infection in calu-3 cells(EC50=0.64± 0.16 μM).

Hemolytic Activity No hemolysis information or data found in the reference(s) presented in this entry

Cytotoxicity

[Ref.29442512]Calu-3 cell:CC50>100 μM

Binding Target membrane

Mechanism The peptide inhibits MERS-CoV infection and its spike (S) protein-mediated cell–cell fusion.

Structure Information

PDB ID None

Predicted Structure Download DRAVPe00573

Linear/Cyclic Linear

N-terminal Modification Acetylation

C-terminal Modification Amidation

Other Modification None

Stereochemistry L

Physicochemical Information

Formula C193H321N43O64S

Absent amino acids ACFGHPRW

Common amino acids L

Mass 4299.98

Pl 4.48

Basic residues 5

Acidic residues 9

Hydrophobic residues 12

Net charge -4

Boman Index -6020

Hydrophobicity -40.56

Aliphatic Index 124.44

Half Life

Mammalian:1.9 hour
Yeast:>20 hour
E.coli:>10 hour

Extinction Coefficient cystines 2980

Absorbance 280nm 85.14

Polar residues 8

Literature Information

Literature 1

Title Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors.

Pubmed ID 29442512

Reference J Med Chem. 2018 Mar 8;61(5):2018-2026.

Author Wang C, Xia S, Zhang P, Zhang T, Wang W, Tian Y, Meng G, Jiang S, Liu K.

DOI 10.1021/acs.jmedchem.7b01732